scholarly journals Bioactive Self-Nanoemulsifying Drug Delivery Systems (Bio-SNEDDS) for Combined Oral Delivery of Curcumin and Piperine

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1703 ◽  
Author(s):  
Mohsin Kazi ◽  
Ahmad A. Shahba ◽  
Saad Alrashoud ◽  
Majed Alwadei ◽  
Abdelrahman Y. Sherif ◽  
...  

Background: Bioactive oils of natural origin have gained huge interests from health care professionals and patients. Objective: To design a bioactive self-nanoemulsifying drug delivery system (Bio-SNEDDS) comprising curcumin (CUR) and piperine (PP) by incorporating bioactive natural oils in the formulation. Methods: The self-emulsifying properties of apricot, avocado, black seed and Zanthoxylum rhetsa seed oils were screened within various SNEDDS formulations. Each liquid SNEDDS formulation was loaded with both CUR and PP. The optimal liquid SNEDDS were solidified using Aeroperl® and Neusilin® at 1:1 w/w ratio. Liquid and solid SNEDDS were characterized by droplet size analysis, equilibrium solubility, scanning electron microscopy, X-ray powder diffraction, differential scanning calorimetry, and Fourier transform infrared spectroscopy. In-vitro dissolution studies were performed to evaluate the efficiency of CUR and PP release from solid Bio-SNEDDS. Results: The liquid SNEDDS comprised of black seed oil exhibited excellent self-emulsification performance, low droplet size along with transparent appearance. The inclusion of the cosolvent Transcutol P improved the solubilization capacity of both CUR and PP. The liquid SNEDDS were efficiently solidified using the two adsorbents and presented the drugs within amorphous state. In particular, SNEDDS comprised of black seed oil/Imwitor988/Transcutol P/Cremophor RH40 (20/20/10/50) and when solidified with Neusilin showed enhanced CUR and PP release (up to 60% and 77%, respectively). In addition, this formulation efficiently delivers the highly bioactive black seed oil to the patient. Conclusions: The optimized Bio-SNEDDS comprising black seed oil showed outstanding self-emulsification characteristics along with enhanced CUR/PP dissolution upon solidification.

2020 ◽  
Vol 1469 ◽  
pp. 012022
Author(s):  
S E Priani ◽  
S S Maulidina ◽  
F Darusman ◽  
L Purwanti ◽  
D Mulyanti

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1107
Author(s):  
Mohsin Kazi ◽  
Fahd A. Nasr ◽  
Omar Noman ◽  
Abdulrahman Alharbi ◽  
Mohammed S. Alqahtani ◽  
...  

Curcumin (CUR) is an attractive polyphenol for its anti-inflammatory, antibacterial, antioxidant, and anticancer properties. Poor solubility in water and sensitivity against sunlight are the most challenging characteristics in the development of CUR for clinical use. The aim is to develop oral lipid-based bioactive self-nanoemulsifying drug delivery systems (Bio-SNEDDSs) for curcumin as a candidate for cancer therapy. Bio-SNEDDSs containing black seed oil, medium-chain mono- and diglycerides, and surfactants were prepared as CUR delivery vehicles. The morphology, droplet size, physical stability, encapsulation efficiency, risk of precipitation, lipid digestion, antioxidant activity, and antimicrobial activity were evaluated for the representative formulations. Finally, an MTT assay was performed on MCF-7 cells to determine the cytotoxic effect of the different formulations. The results showed lower droplet size (28.53 nm) and higher drug-loading (CUR 20 mg, thymoquinone 1.2 mg) for the representative Bio-SNEDDS (black seed oil/Imwitor 988/KolliphorEL (35/15/50) % w/w), along with a transparent appearance upon aqueous dilution. The dynamic dispersion and in-vitro lipolysis data proved that the Bio-SNEDDS was able to keep the CUR in a solubilized form in the gastrointestinal tract. From the antioxidant and antimicrobial studies, it was suggested that the Bio-SNEDDS had the highest activity for disease control. The MTT assay showed that the representative Bio-SNEDDS treatment led to a reduction of cell viability of MCF-7 cells compared to pure CUR and conventional SNEDDSs. A Bio-SNEDDS with elevated entrapment efficiency, antioxidant/antimicrobial activities, and an antiproliferative effect could be the best anticancer drug candidate for potential oral delivery.


2021 ◽  
Vol 11 (10) ◽  
pp. 1746-1751
Author(s):  
Shaiqah Mohd Rus ◽  
Farahidah Mohamed ◽  
Mohd. Rushdi Abu Bakar ◽  
Abd Almonem Doolaanea ◽  
Awis Sukarni Mohmad Sabere

Black seed oil (BSO) contains thymoquinone, an active ingredient that is well-known for its antioxidant property. The bitter taste of BSO makes it challenging for the consumers, mainly children and the elderly, to consume it every day. Thus, BSO is encapsulated in alginate beads in micrometre size to enhance its palatability. This encapsulation was previously established in the lab-scale and the standard mixing method to produce a stable BSO-alginate emulsion used a magnetic stirrer coupled with a sonicator. This mixing method is not suitable for the production of BSO beads at a large scale. Hence, this research aims to investigate the impacts of various mixing methods coupled with sonication towards the BSO-alginate emulsion attributes. Four BSOalginate coarse emulsions were prepared using a magnetic stirrer (MS) as the benchmark, overhead stirrer (OS), homogeniser (H), and overhead stirrer combined with homogeniser (OSH). All the coarse emulsions were then sonicated to produce a nanoemulsion using a flow cell sonicator. The coarse emulsions were characterised in terms of dissolution time while the nanoemulsions were characterised in terms of droplet size, polydispersity index, zeta potential, conductivity and absorbance. These characteristics were statistically compared to the benchmark emulsion characteristics. MS, OS, H, and OSH coarse emulsion formation required 45, 230, 102, and 46 minutes to be produced, respectively. There were significant differences (p <0.05) between the droplet size of OSH (266.53±4.36) nm and MS (285.50±1.15) nm emulsions, indicating that the OSH emulsion was more stable. The absorbance of OSH BSO-alginate nanoemulsion was significantly lower (p <0.05) than the benchmark. In comparison to MS as the benchmark, OSH technique produced a stable emulsion in terms of lower dissolution time, droplet size, zeta potential, and absorbance.


2019 ◽  
Vol 6 (2) ◽  
pp. 57
Author(s):  
Sani Ega Priani ◽  
Wulan Kartika Dewi ◽  
Amila Gadri

<p align="center"><strong>Abstrak</strong></p><p align="center"><strong> </strong></p><p class="Default">Jerawat adalah penyakit kulit yang paling sering terjadi dan timbul akibat penyumbatan atau inflamasi pada kelenjar pilosebasea. <em>Propionibacterium acnes </em>diketahui merupakan bakteri utama pemicu terjadinya inflamasi pada jerawat. Minyak jinten hitam dan minyak zaitun diketahui memiliki aktivitas antibakteri sehingga dapat dikembangkan untuk pengobatan jerawat karena infeksi. Penelitian ini bertujuan untuk menguji aktivitas antibakteri kombinasi minyak jinten hitam dan minyak zaitun terhadap <em>P. acnes</em> dan memformulasikannya ke dalam bentuk sediaan mikroemulsi gel. Pengujian aktivitas antibakteri dilakukan dengan metode difusi agar pada konsentrasi kombinasi minyak 0,25; 0,5; dan 1%. Formulasi sediaan mikroemulsi gel dilakukan dengan menggunakan <em>cremophor RH </em>40 sebagai surfaktan, gliserin sebagai kosurfaktan, dan viscolam mac 10 sebagai <em>gelling agent</em>. Karakterisasi sediaan meliputi pengujian organoleptis, pH, viskositas, sifat alir, ukuran globul, dan stabilitas termodinamik. Hasil penelitian menunjukkan bahwa konsentrasi minyak 0,5% sudah memberikan aktivitas antibakteri terhadap <em>P. acnes</em> dengan diameter hambat 12,47±1,07mm. Formula optimum mikroemulsi gel adalah formula yang mengandung minyak (6%), <em>cremophor RH </em>40 (35%), gliserin (35%), dan gel viskolam 20%. Sediaan mikroemulsi gel memiliki rata rata ukuran globul 120 nm yang memenuhi persyaratan ukuran globul mikroemulsi. Sediaan mikroemulsi gel stabil berdasarkan hasil uji stabilitas termodinamik dengan tidak terlihat adanya pemisahan fase.</p><p><strong> </strong></p><p><strong>Kata kunci</strong> :   Minyak jinten hitam, Minyak zaitun, <em>P</em><em>.</em><em> acnes</em><em>, </em>Mikroemulsi gel</p><p> </p><p align="center"><strong><em>Formulation of anti acne microemulsion gel containing combination of black seed oil </em></strong><strong><em>(Nigella sativa L.) </em></strong><strong><em> and olive oil </em></strong><strong><em>(Olea europaea L.)</em></strong><strong><em> </em></strong></p><p align="center"><strong><em> </em></strong></p><p align="center"><strong><em>Abstract</em></strong><strong><em></em></strong></p><p align="center"><strong><em> </em></strong></p><p><em>Acne vulgaris is the most common </em><em>skin disease involving blockage and/or inflammation of pilosebaceous unit. </em><em>Propionibacterium acnes</em><em>  has</em><em> been recognized as pus-forming bacteria triggering an inflammation in acne</em><em>. Black seed and olive oil are herbal medicines that known have antibacterial activity, that could be develop for acne treatment. </em><em>This research was conducted to determine antibacterial activity of black seed and olive oil </em><em>combination</em><em> against P. acnes and </em><em>develop the microemulsion gel preparation containing of the oil. </em><em>Antibacterial activity test was conducted by agar diffusion method at concentration at 0,25; 0,5; and 1% of oil combination. </em><em>Microemulsion gel was made using </em><em>cremophor RH 40 as surfactant, </em><em>glycerine as </em><em>cosurfactant, and viscolam mac 10</em><em> as </em><em>gelling agent.  Microemulsion gel was evaluated by organoleptic, pH, rheologycal properties,</em><em> spreadability, droplet size, and  </em><em> thermodinamic  stabilitiy test. The result showed that concentration 0,5% of oil combination</em><em> has antibacterial activity </em><em>towards P. acnes </em><em>with inhibitory diameter </em><em>12,47 </em><em>± 1,069</em><em> </em><em>mm. Optimum formula microemulsion gel with the finest characteristic, containing the oil combination </em><em>(6%), cremophor RH 40  (35%), gliserin  (35%), and  viscolam</em><em> gel </em><em> 20%. The</em><em> average of</em><em> droplet size microemulsion gel is 120</em><em> </em><em>nm and those size are qualify with the droplet size of microemulsion.</em><em> The microemulsion gel was stabile based on </em><em>thermodinamic</em><em> stability</em><em> tests without phase separation.</em><strong><em></em></strong></p><p><strong><em> </em></strong></p><p class="Default"><strong><em>Keywords</em></strong><em>:       black seed oil, olive oil, P. acnes, microemulsion gel</em></p>


2021 ◽  
Vol 78 ◽  
pp. 104391
Author(s):  
Shimul Halder ◽  
Amena Islam ◽  
Md. Abdul Muhit ◽  
Manik Chandra Shill ◽  
Syed Shabbir Haider

Author(s):  
Sani Ega Priani ◽  
Septiani Siti Maulidina ◽  
Fitrianti Darusman

Aims: The aims of this research were to develop and characterize liquid and solid micro emulsifying drug delivery system (L-SMEDDS and S-SMEDDS) containing black seed oil.  Study Design: Experimental Research Design (laboratory). Place and Duration of Study: The study was conducted at research laboratory of pharmacy department UNISBA, between August 2018- August 2019. Methodology: The optimization of L-SMEDDS was carried out using various comparison of oil, surfactant, and cosurfactant. All formulations were evaluated for percent transmittance, emulsification time, dispersibility, robustness, and thermodynamic stability. The best formula of L-SMEDSS was evaluated for globule size distribution and converted to S-SMEDDS by spray drying method using aerosil 200 as adsorbent. S-SMEDDS were evaluated for organoleptic, flowability, compressibility, emulsification time, dispersibility, robustness and surface morphology. Results: The best formula of L-SMEDDS contains tween 80 as a surfactant and PEG 400 as cosurfactant (2:1) with a ratio of oil and Smix (2:8). The L-SMEDDS preparation meets the requirement of percent transmittance (95.77%), emulsification time (37.67 seconds), grade A of dispersibility, stable of robustness and thermodynamics study with the average of globule size was 231 nm. S-SMEDDS preparation meets the requirement of the moisture content, flowability, emulsification time, and stable on robustness testing with a spherical shape. Conclusion: L-SMEDDS and S-SMEDDS of black seed oil have been developed and have good physical characteristics and stability.


2020 ◽  
Vol 9 (4) ◽  
pp. 233
Author(s):  
Kurdman Sulaiman ◽  
Ihsan T. Tayeb

This study was performed to determine the percentage of hatchability, post-hatch growth performance, and immune response of broiler subjected to in-ovo injection of some natural oils. A total of 360 eggs of ross broiler strain were obtained. Eggs were distributed into six groups: T1,Negative Control (No injection), T2, positive control (injected with 0.1 ml distilled water; T3 injected with 0.1ml of rosemary oil ; T4, injected with 0.1ml of black seed oil; T5 injected with 0.1 ml of olive oil, and T6, injected with 0.1 ml of almond oil. The newly hatched chicks were distributed into 6 groups of 4 replicates of 10 chick. Higher hatchability percentage was found in rosemary oil, followed by almond oil and olive oil –injected eggs. The final weights of birds that were hatched from rosemary oil, and black seed oil -injected groups were significantly (P < 0.05) higher than other experimental groups. Feed intake and feed conversion ratio were improved with in -ovo administration of rosemary oil and black seed oil. In addition, the level of blood cholesterol and blood glucose were decreased (p<0.05) in birds from all-natural oils-injected eggs. The level of IgM and IgG was significantly (p<0.05) increased in the serum of birds that were hatched from natural oils injected eggs. It could be concluded that in-ove injection of natural oils used in this study was promising to increase the hatchability percentage and improve the subsequent growth and immune responses of post hatched birds.


2021 ◽  
pp. 29-31
Author(s):  
Seval Kaya ◽  
Yusuf Nergiz ◽  
Firat Asir

In this study, it was aimed to investigate the protective effect of black seed oil against testicular tissue damage in diabetic rats. A total of 18 male rats were divided into 3 groups, including 6 rats in each group.Groups; control (n=6), diabetes (n=6), diabetes + black seed oil (n=6). A single dose of 45 mg / kg streptozocine (STZ) was injected intraperitoneally to induce diabetes. Diabetes + Black seed oil group: For 56 days, 2.5 ml / kg of black seed oil was administered orally to rats.The rats were sacriced at the end of 56 days. Testicular tissues were taken for routine parafn tissue processing for histopathological examination. Parafn sections were stained with Hematoxylin-Eosin and PAS and examined under a light microscope. Atrophy and degeneration were observed in the seminiferous tubules of diabetic group. Histology of black seed oil group sections were similar to that of control group. A signicant difference was found between the black seed oil group and the diabetes group in terms of blood glucose values. As a result, we think that Black Seed Oil ameliorates to the tissue damage caused by diabetes and the decrease in blood sugar value.


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